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01-07-2020 | Combustion | Original Article

Evaluation of carboxamide-type synthetic cannabinoids on the functional activities at cannabinoid receptors and biological effects via inhalation exposure test

Authors: Akihiro Takeda, Takahiro Doi, Akiko Asada, Toshinari Suzuki, Katsuhiro Yuzawa, Hiroshi Ando, Yoshikazu Kubo, Akemichi Nagasawa, Fujifumi Kaihoko, Yuko Hasegawa, Kazuyoshi Tanaka, Kai Igarashi, Tomokazu Maeno, Atsuko Suzuki, Seiko Shimizu, Nozomi Uemura, Jun’ichi Nakajima, Jin Suzuki, Takaomi Tagami

Published in: Forensic Toxicology | Issue 2/2020

Abstract

Purpose

Three synthetic carboxamide-type cannabinoids (5F-MDMB-PICA, 5F-EMB-PINACA, and AMB-CHMICA) were evaluated in terms of their in vitro activities at the cannabinoid receptors CB₁ and CB₂ and in vivo biological effects when smoking the synthetic cannabinoids to assess their biological effects.

Methods

[³⁵S]Guanosine-5′-O-(3-thio)-triphosphate binding assays were performed to investigate the half maximal effective concentration values of the test compounds at the CB₁ and CB₂ receptors. Additionally, the biological effects were evaluated by observing and scoring the behavior of mice with equipment in which they inhaled smoke from a herbal mixture containing the test compounds.

Results

All three synthetic cannabinoids tested in this study activated the CB₁ and CB₂ receptors in vitro. 5F-MDMB-PICA showed less than 1 nM of the half maximal effective concentration value for both receptors. Therefore, it was suggested that 5F-MDMB-PICA was the strongest CB₁ and CB₂ receptor agonist in comparison with synthetic cannabinoids evaluated in the past. The degree of the various biological effects, specifically passivity, spontaneous activity, abnormal gait, abnormal position, and grip strength, when smoking the synthetic cannabinoids corresponded to the functional activity at the CB₁ receptor. However, some biological effects differed between 5F-MDMB-PICA and 5F-MDMB-PINACA, used as a positive control, and AMB-CHMICA induced some biological effects in contrast to the other tested synthetic cannabinoids.

Conclusion

This study provides information regarding the biological effects when smoking synthetic cannabinoids from the functional activities at the CB₁ and CB₂ receptors, considering their way of inhalation and thermal degradation.

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Title: Evaluation of carboxamide-type synthetic cannabinoids on the functional activities at cannabinoid receptors and biological effects via inhalation exposure test
Authors: Akihiro Takeda
Takahiro Doi
Akiko Asada
Toshinari Suzuki
Katsuhiro Yuzawa
Hiroshi Ando
Yoshikazu Kubo
Akemichi Nagasawa
Fujifumi Kaihoko
Yuko Hasegawa
Kazuyoshi Tanaka
Kai Igarashi
Tomokazu Maeno
Atsuko Suzuki
Seiko Shimizu
Nozomi Uemura
Jun’ichi Nakajima
Jin Suzuki
Takaomi Tagami
Publication date: 01-07-2020
Publisher: Springer Singapore
Keywords: Combustion
Cannabinoid
Pica Syndrome
Combustion
Published in: Forensic Toxicology / Issue 2/2020
Print ISSN: 1860-8965
Electronic ISSN: 1860-8973
DOI: https://doi.org/10.1007/s11419-020-00534-x

At a glance: The STEP trials

Springer Medicine

Evaluation of carboxamide-type synthetic cannabinoids on the functional activities at cannabinoid receptors and biological effects via inhalation exposure test

Abstract

Purpose

Methods

Results

Conclusion

At a glance: The STEP trials

Springer Medicine

Abstract

Purpose

Methods

Results

Conclusion

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